Studies on the Antioxidant and Cytotoxic Potentials of the Peel Extract of Dacryodes rostrata

Breast cancer is one type of cancer that causes the highest death in women in Indonesia. Alternative herbal-based cancer treatments have been developed, one of which is using fruits. Dacryodes rostrata, a fruit commonly consumed by residents in Kalimantan, is rich in antioxidants such as flavonoids and phenolics. The purpose of this study was to determine the value of antioxidant and cytotoxic activity of water and ethanol extract of D. rostrata peel against T-47D breast cancer cell lines. The fruit extraction was carried out by using maceration method. Antioxidant activity test using 2,2-diphenyl-1-picrylhydrazyl (DPPH) method and cytotoxic test using MTT method (3-(4,5-dimethylthiazole-2-yl)-2,5-diphenitetrazolium bromide) assay. The results showed that D. rostrata water and ethanol extract had antioxidant activity with IC50 values 121.7 ppm and 59.27 ppm, respectively. While cytotoxic effect on T-47D cells with IC50 values of 322.55 ppm and 143.02 ppm, respectively. This study showed that D. rostrata peel water extract had moderate antioxidant activity and moderate cytotoxic effect against T-47D breast cancer cells in vitro which could be used as a chemo preventive to prevent and inhibit cancer cell growth.

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Biotinylated xanthohumol: synthesis and in vitro biological evaluation for anticancer therapy

10.20944/preprints201807.0039.v1 ◽

2018 ◽

Author(s):

Monika Stompor ◽

Rafał Podgórski ◽

Marta Świtalska ◽

Joanna Wietrzyk

Keyword(s):

Breast Cancer ◽

Antioxidant Activity ◽

Cancer Cells ◽

Cell Lines ◽

Biological Evaluation ◽

Breast Cancer Cell Lines ◽

Dpph Method ◽

Ic50 Values ◽

Mcf 7

Two biotinylated derivatives of the main hop chalcone xanthohumol (1) were prepared by a one-step synthesis via esterification using biotin and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC HCl) and 4-dimethylaminopyridine (DMAP) as coupling reagents. The products were characterized spectroscopically and their antiproliferative activity toward MCF-7, MCF-10A, HepG2, MDA-MB-231, 4T1 and Balb/3T3 cell lines was investigated using the SRB assay. For all three tested compounds the best activity was noted in the case of human (MCF-7) and mice (4T1) breast cancer cell lines (IC50 values < 9 μM). Both biotinylated derivatives showed higher anticancer activity than xanthohumol (1) towards all types of tested breast cancer cells. Double biotinylated xanthohumol (3) proved to be the most active in inhibiting cell growth, with IC50 values equal to 5.35 ± 1.5 μM for 4T1 and 8.03 ± 0.53 µM for MCF-7 cell lines. Compound 3 was also more active than 1 and 2 against liver cancer cells HepG2 (IC50 = 17.37 ± 5.1 μM), while the IC50 values for 1 and 2 were equal to 21.5 ± 2.7 and 22.1 ± 3.9 µM, respectively. 4‑O‑biotinylxanthohumol (2) was the second most active growth inhibitor, particularly with respect to MCF-7 (IC50 = 6.19 ± 1.7 μM) and 4T1 (IC50 = 6.64 ± 0.4 μM) cell lines. The antioxidant activity was evaluated using the 1.1-diphenyl-2-picrylhydrazyl radical (DPPH) method. All tested compounds (1-3) have antioxidant activity between 2.73 and 3.38 mM. It was reported for the first time that new prenylated chalcones containing the biotin moiety effectively inhibited proliferation of cancer cells in vitro.

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SYNTHESIS, CYTOTOXIC EVALUATION AND MOLECULAR DOCKING STUDIES OF NEW 3-(1,3,4-OXADIAZOLYL)-QUINOLINONE DERIVATIVES AGAINST BREAST CANCER CELL LINES

INDIAN DRUGS ◽

10.53879/id.55.11.11472 ◽

2018 ◽

Vol 55 (11) ◽

pp. 19-31

Author(s):

S Muthadi ◽

◽

R. Guda ◽

M. Kasula ◽

A Garlapati ◽

...

Keyword(s):

Breast Cancer ◽

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Cancer Cell Lines ◽

Docking Studies ◽

Breast Cancer Cell Lines ◽

Dpph Method

A series of new substituted 3-(5-substituted-1,3,4-oxadiazol-2-yl)-4(1H)-quinolinone derivatives (5a-t) have been designed and synthesized using appropriate protocols. All of them were screened for cytotoxic activity against human breast cancer cell lines (MCF-7 and T47D) and antioxidant activity (DPPH method). Among them, 5f exhibited promising inhibitory activity with IC50 values 7.429 and 8.388 against the two cell lines chosen. The molecular interactions with target (aromatase receptor by docking) were found to correlate well with in vitro cytotoxic activity, i.e. 5f showed the high binding affinity -12.34 kcal/ mol. In the antioxidant screening also, 5f and 5h were found superior to others.

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In vitro potentiation by lonidamine of the cytotoxic effect of adriamycin on primary and established breast cancer cell lines

Breast Cancer Research and Treatment ◽

10.1007/bf01832355 ◽

1992 ◽

Vol 24 (1) ◽

pp. 27-34 ◽

Cited By ~ 12

Author(s):

Saverio Savini ◽

Wainer Zoli ◽

Oriana Nanni ◽

Annalisa Volpi ◽

G. Luca Frassineti ◽

...

Keyword(s):

Breast Cancer ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Cytotoxic Effect ◽

Cancer Cell Lines ◽

Breast Cancer Cell Lines

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ANTITUMOR EFFECT OF SUNITINIB AND BORTEZOMIB ON BREAST CANCER CELL LINE IN VITRO

Problems in oncology ◽

10.37469/0507-3758-2017-63-1-141-145 ◽

2017 ◽

Vol 63 (1) ◽

pp. 141-145

Author(s):

Yuliya Khochenkova ◽

Eliso Solomko ◽

Oksana Ryabaya ◽

Yevgeniya Stepanova ◽

Dmitriy Khochenkov

Keyword(s):

Breast Cancer ◽

Cell Line ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Antitumor Effect ◽

Cancer Cell Lines ◽

Breast Cancer Cell Lines ◽

Actual Problem

The discovery for effective combinations of anticancer drugs for treatment for breast cancer is the actual problem in the experimental chemotherapy. In this paper we conducted a study of antitumor effect of the combination of sunitinib and bortezomib against MDA-MB-231 and SKBR-3 breast cancer cell lines in vitro. We found that bortezomib in non-toxic concentrations can potentiate the antitumor activity of sunitinib. MDA-MB-231 cell line has showed great sensitivity to the combination of bortezomib and sunitinib in vitro. Bortezomib and sunitinib caused reduced expression of receptor tyrosine kinases VEGFR1, VEGFR2, PDGFRa, PDGFRß and c-Kit on HER2- and HER2+ breast cancer cell lines

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Small Molecular Leads Differentially Active Against HER2 Positive and Triple Negative Breast Cancer Cell Lines

Medicinal Chemistry ◽

10.2174/1573406414666181106143912 ◽

2019 ◽

Vol 15 (7) ◽

pp. 738-742 ◽

Cited By ~ 1

Author(s):

Adnan Badran ◽

Atia-tul-Wahab ◽

Sharmeen Fayyaz ◽

Elias Baydoun ◽

Muhammad Iqbal Choudhary

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Triple Negative ◽

Cancer Cell Lines ◽

Breast Cancer Cell Lines ◽

Cancer Type

Background:Breast cancer is the most prevalent cancer type in women globally. It is characterized by distinct subtypes depending on different gene expression patterns. Oncogene HER2 is expressed on the surface of cell and is responsible for cell growth regulation. Increase in HER2 receptor protein due to gene amplification, results in aggressive growth, and high metastasis in cancer cells.Methods:The current study evaluates and compares the anti-breast cancer effect of commercially available compounds against HER2 overexpressing BT-474, and triple negative MDA-MB-231 breast cancer cell lines.Results:Preliminary in vitro cell viability assays on these cell lines identified 6 lead molecules active against breast cancer. Convallatoxin (4), a steroidal lactone glycoside, showed the most potent activity with IC50 values of 0.63 ± 0.56, and 0.69 ± 0.59 µM against BT-474 and MDA-MB-231, respectively, whereas 4-[4-(Trifluoromethyl)-phenoxy] phenol (3) a phenol derivative, and Reserpine (5) an indole alkaloid selectively inhibited the growth of BT-474, and MDA-MB-231 breast cancer cells, respectively.Conclusion:These results exhibited the potential of small molecules in the treatment of HER2 amplified and triple negative breast cancers in vitro.

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The α2δ1 subunit of the voltage-gated calcium channel as a potential candidate for breast cancer tumor initial cells biomarker

Cancer Biomarkers ◽

10.3233/cbm-203165 ◽

2021 ◽

pp. 1-11

Author(s):

Meng Li ◽

Wenmin Zhang ◽

Xiaodan Yang ◽

Guo An ◽

Wei Zhao

Keyword(s):

Breast Cancer ◽

Cancer Cells ◽

Cell Lines ◽

Cancer Cell ◽

Breast Cancer Cell ◽

Breast Cancer Cells ◽

Cancer Cell Lines ◽

Breast Cancer Cell Lines ◽

Self Renewal

BACKGROUND: The voltage-gated calcium channel subunit alpha 2 delta 1 (α2δ1) is a functional tumor initial cells (TICs) marker for some solid cancer cells. This study aimed to investigate whether α2δ1 can be used as a potential TIC marker for breast cancer cells. METHODS: α2δ1+ and α2δ1- cells were identified and sorted from the breast cancer cell lines MDA-MB-231, MDA-MB-435s and ZR-75-1 by Immunofluorescence (IF) and Fluorescent-activated cell sorting (FACS) analyses. Spheroid formation in vitro and tumorigenesis in NOD/SCID mice were assessed to determine the self-renewal and serial transplantation abilities of these cells. Using a lentivirus infection system for α2δ1 in breast cancer cell lines, we determined the mRNA levels of stemnessassociated genes by quality real-time PCR (qRT-PCR). Boyden chamber and wounding assays were further performed to detect the migration of α2δ1 overexpression cells. Bioinformatics explored the relationship of molecular classification of breast cancer and drug resistance. RESULTS: α2δ1 presents on the cytomembrane of breast cancer cells, with a positive rate of 1.5–3%. The α2δ1+ cells in breast cancer cell lines have a stronger self-renewal ability and tumor initiating properties in vitro and in vivo. Overexpressing α2δ1 successfully enhanced the sphere-forming efficiency, and upregulated the expression of stemness-associated genes, and increased cell migration. However, seldom significant was available between estrogen receptor +/- (ER+/-), progesterone receptor (PR+/-), and Her2+/-. CONCLUSIONS: Breast cancer cells positive for the α2δ1 charactered tumor initiation, and α2δ1 is a potential TIC marker for breast cancer that further promotes the migration.

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